Calcipotriol monohydrate

SKU: orb1296103

Description

Calcipotriol monohydrate is a synthetic vitamin D3 analog that binds with high affinity to the vitamin D receptor. It is widely used in psoriasis research, facilitating both in vitro mechanistic studies and in vivo models of skin inflammation and keratinocyte proliferation.

Research Area

Metabolism Research

Key Properties

• CAS Number: 147657-22-5
• MW: 430.62
• Purity: 99.95% (May vary between batches)
• Formula: C₂₇H₄₂O₄
• SMILES: O.[H][C@@]12CC[C@H]([C@H](C)\C=C\[C@@H](O)C3CC3)[C@@]1(C)CCC\C2=C/C=C1/C[C@@H](O)C[C@H](O)C1=C
• Target: Vitamin
• Solubility: Ethanol:95 mg/mL (220.61 mM);DMSO:95 mg/mL (220.61 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.66 mM)

Bioactivity

• In Vivo:
  The weight gain is significantly smaller in the groups treated with Diclofenac plus Calcipotriol monohydrate (p=0.018) and Diclofenac plus DFMO plus Calcipotriol monohydrate (p=0.002) compare with placebo (linear regression model).
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• In Vitro:
  Calcipotriol monohydrate (100, 10, and 1 ng/mL) significantly upregulated the expression of NKp30 on the surface of NK cells after 4 h incubation. When NHEK cells are not stimulated with IL-17A or IL-22, Calcipotriol monohydrate slightly enhances (0.2 nM) IL-8 mRNA expression or has no effect (2-20 nM). The addition of IL-17A and IL-22 markedly increased the mRNA expression of IL-8, confirming our previous study. This enhanced IL-8 mRNA expression is suppressed by Calcipotriol monohydrate (2, 20 and 40 nM) in a dose dependent manner.
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• Cell Research:
  Normal human epidermal keratinocytes are grown in serum-free keratinocyte growth medium Epilife and used at the third passage in all experiments. The growth supplement is omitted 48 h before experiments. As a control, IL-17A and IL-22 are either added or not added to the cells. Cultured NHEK cells are stimulated with IL-17A (200 ng/mL) and/or IL-22 (200 ng/mL) followed by co-incubation in the presence or absence of Calcipotriol at 0.2-40 nM to test its modulatory effect. Cells are harvested 3 days later and subjected to real-time qPCR. Culture supernatants are also collected and frozen at -80°C until used for ELISA .
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• Animal Research:
  The 160 female SKH-1 hairless mice (6-7 weeks of age) are used. After UV treatment, mice without tumors are randomly divided into five groups, four chemoprevention groups (Diclofenac plus DFMO; Diclofenac plus Calcipotriol; DFMO plus calcitriol; and Diclofenac plus DFMO plus Calcipotriol) and one placebo group (skin lotion). The mice are treated with test mixtures once a day, five days a week, for a total of 17 weeks. The test mixtures are applied topically on the dorsal surface of the mice. Ten microliters are applied by a pipette after which the mixture is rubbed onto the skin. This corresponded to the following doses of each active substance in the treatments: 100 μg/week for Diclofenac (30 mg/g undiluted), 0.166 μg/week for Calcitriol (50 μg/g undiluted), and 463.3 μg/week for DFMO (139 mg/g undiluted) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Calcipotriol, Calcipotriol monohydrate, Calcipotriol Monohydrate, Inhibitor, inhibit, VD/VDR, Vitamin D, Vitamin D receptor, vitamin D receptor

Compound Identifiers

PubChem CID

49800068